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    • 10. 发明申请
    • Direct Compression Formulation and Process
    • 直接压缩配方和工艺
    • US20080193529A1
    • 2008-08-14
    • US11916490
    • 2006-06-08
    • James KowalskiJay Parthiban LakshmanArun Patel
    • James KowalskiJay Parthiban LakshmanArun Patel
    • A61K9/20A61K31/4439A61K9/14A61K31/40
    • A61K31/40A61K31/4439A61K45/06A61K2300/00
    • Dipeptidylpeptidase IV inhibitor (herein referred to as DPP-IV) that may be 98.5-100% pure is a high-dose drug capable of being directly compressed with a glitazone and specific excipients into sold form dosage forms, such as tablets and capsules having desired, hardness, disintegrating ability and acceptable dissolution characteristics. DPP-IV is not inherently compressible and thus presents formulation problems. Excipients used in the formulation enhance the flow and compaction properties of the drug and tableting mix. Optimal flow contributes to uniform die fill and weight control. The binder used ensures sufficient cohesive properties that allow DPP-IV to be compressed using the direct compression method. The tablets produced provide an acceptable in vitro dissolution profile.
    • 可以为98.5-100%纯度的二肽基肽酶IV抑制剂(在本文中称为DPP-IV)是能够用格列酮和特定赋形剂直接压制成销售形式的剂型的高剂量药物,例如具有期望的片剂和胶囊 ,硬度,崩解性和可接受的溶解特性。 DPP-IV不是固有的可压缩性,因此呈现配方问题。 制剂中使用的赋形剂增强了药物和压片混合物的流动和压实性能。 最佳流量有助于均匀的模头填充和重量控制。 使用的粘合剂确保足够的内聚性质,使DPP-IV能够使用直接压缩方法进行压缩。 所制备的片剂提供可接受的体外溶出曲线。